两个dpa类配体的铜(Ⅱ)配合物的合成、结构、核酸酶活性及细胞毒性（英文）

Two Copper(Ⅱ) Complexes with dpa-Based Ligand:Syntheses,Structures,Nuclease Activity and Cytotoxicity

以dpa衍生配体4-methyl-N,N-bis(pyridin-2-ylmethyl)aniline(L)合成2个单核铜配合物[CuL(NO_3)_2](1)和[CuL(OAc)(H_2O)]ClO_4(2),并对其进行了表征。单晶结构显示,配合物1中的Cu中心可以描述为畸变的五角双锥构型,而2的Cu中心为畸变的八面体构型。运用电子吸收和发射光谱法研究了配合物与CT-DNA的键合作用,结果表明2个配合物与DNA的相互作用均为部分插入模式。通过改变浓度、时间进一步检测配合物切割DNA的能力,以及验证其切割机理,结果表明在外界诱导剂存在下,2个配合物均表现出强的切割DNA的能力,其作用机理为氧化切割机理,其中活性氧可能为·OH和1O_2。利用MTT法测定了配合物对体外HeLa、HepG-2和SGC-7901肿瘤细胞增殖的抑制能力。

Two new mononuclear copper（Ⅱ） complexes,[CuL（NO3）2] （1） and[CuL（OAc）（H2O）]ClO4 （2）, with dpa-based ligand （L=4-methyl-N,N-bis（pyridin-2-ylmethyl）aniline） have been synthesized and characterized by various physico-chemical techniques. The crystal structure of complex 1 displays a distorted pentagonal bipyramidal geometry, and the geometry around copper center of 2 can be described as a distorted octahedron. Interaction of the complexes with CT-DNA has been explored by using absorption and emission spectral methods, and the result suggests that the binding strength of the two complexes with DNA is a medium intercalative mode. The concentration-dependent and time-dependent DNA cleavage activity and the mechanism of DNA cleavage have been investigated, which suggest the DNA cleavage efficiencies of both complexes exhibit remarkable enhancement in the presence of external revulsants, and oxidative mechanism has been demonstrated via the pathway involving both hydroxyl radicals （·OH） and singlet oxygen （1O2） as ROS. The in vitro cytotoxic activity of the complexes has been examined by MTT on three cell lines such as HeLa, HepG-2 and SGC-7901.